688342-78-1
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物理化學(xué)性質(zhì)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2025/02/08 | HY-124691 | D-I03 | 688342-78-1 | 1 mg | 335元 |
2025/02/08 | HY-124691 | D-I03 D-I03 | 688342-78-1 | 5mg | 1200元 |
2025/02/08 | HY-124691 | D-I03 D-I03 | 688342-78-1 | 10mM * 1mLin DMSO | 1320元 |
常見問題列表
Target | Value |
RAD52
(Cell-free assay) | 25.8 μM(Ki) |
D-I03 (0-10 μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner.
D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5 μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%. D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1-deficient cells) indicating low genotoxicity of D-I03.
Cell Proliferation Assay
Cell Line: | Capan-1 (BRCA2 ? ) and UWB1.289 (BRCA1 + ) cells |
Concentration: | 0 μM, 2.5 μM, 5 μM, or 10 μM |
Incubation Time: | On days 1 and 3 |
Result: | Preferentially suppressed the growth of Capan-1 and UWB1.289 cells. |
D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days;
nu/nu
mice) treatment reduces BRCA1-deficient MDA-MB-436 tumor growth. Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs.
Pharmacokinetic and toxicity studies indicates that maximal tolerated dose of D-I03 is ≥50 mg/kg, and t
1/2
is 23.4 hours, resulting in >1 μM maximal concentration in peripheral blood.
Animal Model: | Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells |
Dosage: | 50 mg/kg/day |
Administration: | Intraperitoneal injection; daily; for 7 days |
Result: | Reduced BRCA1-deficient MDA-MB-436 tumor growth. |